1. Epigenetics
  2. Histone Demethylase

Histone Demethylase

There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.

Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.

JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.

Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.

Histone Demethylase 相关产品 (27):

Cat. No. Product Name Effect Purity
  • HY-15648B
    GSK-J4 Inhibitor 98.48%
    GSK-J4 是一种有效的 H3K27me3 demethylase 抑制剂,抑制 KDM6B 和 KDM6A 的活性,IC50 值分别为 8.6 µM 和 6.6 µM。
  • HY-B1496
    Tranylcypromine hemisulfate Inhibitor 99.82%
    Tranylcypromine hemisulfate 是 LSD1 抑制剂,同时也是 MAO 的不可逆、非选择性抑制剂,常用于治疗抑郁症。
  • HY-18632
    GSK2879552 Inhibitor 99.82%
    GSK2879552 是一种可口服的,不可逆的 LSD1 抑制剂,具有抗肿瘤活性。
  • HY-12635
    SP2509 Antagonist 99.38%
    SP2509 是有效的,选择性的 LSD1 拮抗剂,IC50 值为 13 nM。
  • HY-15648
    GSK-J1 Inhibitor 99.90%
    GSK-J1 是 H3K27me3/me2-demethylases JMJD3/KDM6BUTX/KDM6A 的抑制剂,对 KDM6B 的 IC50 值为 60 nM。
  • HY-12304
    IOX1 Inhibitor
    IOX1是2OG oxygenase高效广谱抑制剂,包括JmjC去甲基化酶家族,对KDM4A和KDM3A的IC50值分别为0.6uM和0.1uM。
  • HY-101799
    NCGC00244536 Inhibitor 98.57%
    NCGC00244536是高效的KDM4A抑制剂,IC50值为10 nM。
  • HY-104048
    QC6352 Inhibitor
    QC6352 是一种有效的 KDM4C 抑制剂,其 IC50 值为 35 nM。
  • HY-12782
    ORY-1001 Inhibitor >98.0%
    ORY-1001 (RG-6016)是LSD1抑制剂, 出自WO2013057322A1专利。
  • HY-12725
    ML324 Inhibitor 98.19%
    ML324是JMJD2去甲基酶抑制剂,被证实有抗病毒作用。
  • HY-13953
    JIB-04 Inhibitor
    JIB-04 是 Jumonji 组蛋白去甲基酶 (Jumonji histone demethylase) 广谱抑制剂,能抑制 JARID1A,JMJD2E,JMJD3,JMJD2A,JMJD2B,JMJD2C 和 JMJD2D 的活性,其 IC50 值分别为 230,340,855,445,435,1100 和 290 nM。
  • HY-100421
    CPI-455 Inhibitor >98.0%
    CPI-455 是一种有效的特异性 KDM5 抑制剂。
  • HY-100422
    KDM5-IN-1 Inhibitor >98.0%
    KDM5-IN-1是高效选择,有口服活性的KDM5抑制剂,IC50值为15.1 nM。
  • HY-13643
    Daminozide Inhibitor
    Daminozide(DMASA; DIMG; B 995)为植物生长调节剂,能选择性抑制KDM2/7 JmjC亚家族。
  • HY-15648A
    GSK-J2 Inhibitor 98.82%
    GSK-J2 是 GSK-J1 的对映异构体,没有特殊活性。GSK-J1 是 H3K27me3/me2-demethylases JMJD3/KDM6BUTX/KDM6A 的抑制剂。
  • HY-100014
    KDM5A-IN-1 Inhibitor 99.76%
    KDM5A-IN-1是组蛋白去甲基化酶抑制剂。
  • HY-19612A
    DDP-38003 dihydrochloride Inhibitor
    DDP-38003 dihydrochloride是新颖有口服活性的KDM1A/LSD1抑制剂,IC50值为84 nM。
  • HY-100744
    AS8351 Inhibitor 99.70%
    AS8351 是一种 KDM5B 抑制剂,可以诱导和维持有活性的染色质标记从而促进心肌细胞样细胞的产生。
  • HY-101928
    KDM4D-IN-1 Inhibitor >98.0%
    KDM4D-IN-1 是一种新型组蛋白赖氨酸去甲基化酶 4D (KDM4D) 抑制剂,IC50 为 0.41±0.03 μM。
  • HY-15313B
    CBB1007 hydrochloride Inhibitor
    CBB1007盐酸盐是组蛋白去甲基化酶LSD1高效底物竞争性抑制剂,细胞可渗透,对hLSD1的IC50值为5.27uM。